JPS58183615A - High dissolubility medicine and manufacture - Google Patents

High dissolubility medicine and manufacture

Info

Publication number
JPS58183615A
JPS58183615A JP57204422A JP20442282A JPS58183615A JP S58183615 A JPS58183615 A JP S58183615A JP 57204422 A JP57204422 A JP 57204422A JP 20442282 A JP20442282 A JP 20442282A JP S58183615 A JPS58183615 A JP S58183615A
Authority
JP
Japan
Prior art keywords
stabilizer
crystal growth
growth inhibitor
active ingredient
present
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP57204422A
Other languages
Japanese (ja)
Other versions
JPH0341444B2 (en
Inventor
ドナルド・イ−・パノツ
オ−エン・アイ・コリガン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
ERAN CORP Ltd
Original Assignee
ERAN CORP Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ERAN CORP Ltd filed Critical ERAN CORP Ltd
Publication of JPS58183615A publication Critical patent/JPS58183615A/en
Publication of JPH0341444B2 publication Critical patent/JPH0341444B2/ja
Granted legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds

Abstract

(57)【要約】本公報は電子出願前の出願データであるた
め要約のデータは記録されません。(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

【発明の詳細な説明】 本発明は高度溶解性を有づる医薬及びその製造法に関す
る。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to highly soluble pharmaceuticals and methods for producing the same.

医薬の溶解性が、該医薬の治療活性を決定する要因であ
ることは、広く知られている。また治療活性は医薬の生
物学的利用性に依存し、これは良好で且つ安全な吸収性
の機能であることも知られている。後者は医薬を形成す
る有効成分の溶解性の程度に依存している。医薬が吸収
される胃Ｉ！管部位は、非常に限定された特定のもので
あり、医薬の貧弱で且つ不完全な溶液は、上記部位に接
触してもその吸収が１．ｆとんどなされず、利用されな
いため、治療活性値も非常に低い値にとどまってしまう
。従って医薬の良好な溶解性は、該医薬に・　とって必
須不可欠なものである。更に医薬の高度溶解性は、必要
に応じた濃厚？１１′ａ形態の製剤化をも可能にする。It is widely known that the solubility of a drug is a factor that determines its therapeutic activity. It is also known that therapeutic activity depends on the bioavailability of the drug, which is a function of good and safe absorption. The latter depends on the degree of solubility of the active ingredients forming the medicament. The stomach where medicines are absorbed! The vascular site is very limited and specific, and a poor and incomplete solution of the drug will be absorbed only 1. Since f is rarely used or used, its therapeutic activity remains at a very low value. Therefore, good solubility of a drug is essential for the drug. Furthermore, the high solubility of pharmaceuticals means that they can be concentrated as needed. It also allows the formulation of the 11'a form.

現在、液剤形態の医薬は、その投与量を容易に変化させ
得、またイれ自身を春色したり、Ｕ味することができ、
また医薬のビヒクルの微粒子化を可能としている。希釈
された医薬は、粘膜と直接接触しこれによって胃粘膜を
局所的に刺激する例えばカシュー、粉末、錠剤、ビル、
その他の剤型よりも、一層刺激性の少ないものである。Currently, medicines in liquid form can be easily varied in dosage, and can be flavored or flavored.
It also makes it possible to make pharmaceutical vehicles into fine particles. The diluted medicines come into direct contact with the mucous membranes and thereby locally irritate the gastric mucosa, such as cashews, powders, tablets, tablets, etc.
It is less irritating than other dosage forms.

また例えば吸湿性の製剤製品や液体共敵性の混合物等の
粉剤乃至カシューの形態にできない場合、液剤形態は不
可欠である。Liquid forms are also essential when it is not possible to form powders or cashews, such as hygroscopic pharmaceutical products or liquid compatible mixtures.

結晶形態（Ｒも安定な形態）が、最も溶解困難であるこ
とは知られている（例えばニュートンＬＪ、Ｍ、ＮＥＷ
ＴＯＮ）によるＭｆｇ、　Ｃｈｅａ＋１ｓｔＡｅｒｏｓ
ｏｌ　　Ｎｅｗｓ、３７　．３３　（１９６６）参照〕
。It is known that the crystalline form (R is also a stable form) is the most difficult to dissolve (e.g. Newton LJ, M, NEW
TON) by Mfg, Chea+1stAeros
ol News, 37. 33 (1966)]
.

従って従来より有効成分を不定形形１１ｉ（アモルファ
ス）で含む医薬の製造が種々試みられている。Therefore, various attempts have been made to produce pharmaceuticals containing active ingredients in an amorphous form 11i (amorphous).

該不定形形態は、結晶形態より溶解性が向上している。The amorphous form has improved solubility than the crystalline form.

しかしながら不定形形態は下記の欠点を有している。す
なわち不定型形態は経時的に徐々に結晶形態に変化し、
特に安定性に欠ける。これは治療用途に利用される物質
としては、非常に重大な欠点である。However, the amorphous form has the following drawbacks. In other words, the amorphous form gradually changes to the crystalline form over time,
Especially lacking in stability. This is a very serious drawback for substances used for therapeutic purposes.

本発明の目的は、高度の溶解性を有し、しかも各種医薬
品として装求される安定性を具備する医薬形態を提供す
ることにある。An object of the present invention is to provide a pharmaceutical form that has a high degree of solubility and also has the stability required for various pharmaceutical products.

本発明によれば、安定剤及び結晶成長抑制剤の存在下で
の微粒子化により得られ、不定形形態を有することを特
徴とする高度溶解性医薬が提供される。According to the present invention, there is provided a highly soluble drug which is obtained by micronization in the presence of a stabilizer and a crystal growth inhibitor and is characterized by having an amorphous morphology.

本発明の好ましい一実ＩＩＭｓ様によれば、安定剤及び
結晶成長抑制剤は、ポリビニルピロリドンから構成され
る。According to a preferred embodiment of the invention, the stabilizer and crystal growth inhibitor are composed of polyvinylpyrrolidone.

本発明の他の好ましい一実施態様によれば、上記安定剤
及び結晶成長抑制剤は、ポリエチレングリフールーポリ
ビニルビロリドンから構成される。According to another preferred embodiment of the invention, the stabilizer and crystal growth inhibitor are composed of polyethylene glyfluor-polyvinyl pyrrolidone.

本発明によれば、上記抑制剤の微粒子化時の濃度は、有
効成分ＩＩ員の１〜５０！量％とされる。According to the present invention, the concentration of the above-mentioned inhibitor when micronized is 1 to 50! of the active ingredient II member. The amount is expressed as %.

微粒子化に先立ち添加される安定剤及び結晶成長抑制剤
の量は、利用する有効成分に応じて適宜決定される。該
有効成分物質が不安定であればあるだ番ノ、また該物質
が結晶化し易ければそれだけ。The amounts of the stabilizer and crystal growth inhibitor added prior to micronization are appropriately determined depending on the active ingredient to be used. If the active ingredient substance is unstable, it is possible, and if the substance is easily crystallized, it is possible.

上記添加量を増大させればよい。The above addition amount may be increased.

本発明では、また上記抑制剤ポリマーは、医薬の微粒子
化に先だって添加されることが必要であり、単独ですな
わち抑制剤を添加することなく微粒子化された有効成分
に、上記抑ｔｉｌｌ剤を混合するのみでは、本発明医薬
に比し溶解性の劣った製品しか収得できない。In the present invention, the inhibitor polymer needs to be added prior to microparticulation of the drug, and the inhibitor polymer is mixed with the active ingredient that has been micronized alone, that is, without adding an inhibitor. However, only a product with inferior solubility compared to the pharmaceutical of the present invention can be obtained.

史に、多くの分析特に示差熱分析を行なった結果、本発
明医薬中の医薬物質の大部分は、医薬物質−ボリビニル
ビロリドンの不定型複合体となっていることが認められ
た。As a result of many analyzes, particularly differential thermal analysis, it has been found that most of the medicinal substance in the pharmaceutical of the present invention is an amorphous complex of medicinal substance-borivinylpyrrolidone.

本発明の他の一面によれば、溶媒中に有効成分、安定剤
及び結晶成長抑制剤を溶解し、必要に応じ加熱後、入口
温度１１０〜１５０℃及び出口温度８０〜１２０℃の条
件下に微粒子化することを特徴とする高度溶解性医薬の
製造法が提供される。According to another aspect of the present invention, the active ingredient, the stabilizer, and the crystal growth inhibitor are dissolved in a solvent, heated if necessary, and then heated at an inlet temperature of 110 to 150°C and an outlet temperature of 80 to 120°C. A method for producing a highly soluble drug is provided, which is characterized in that it is made into fine particles.

本発明方法の好ましい一実施６１様によれば、有効成分
及び上記抑制剤を溶解するための溶媒とじ５− ては、水及び（又は）低分子量アルコール（Ｃ＋〜Ｃｍ
）が利用される。According to a preferred embodiment 61 of the method of the present invention, a solvent for dissolving the active ingredient and the above-mentioned inhibitor 5- and/or water and/or a low molecular weight alcohol (C+ to Cm
) is used.

以下、本発明を更に詳しく説明するため、本発明に従う
新規な医薬の製造法及びこれにより得られる製品の諸物
性を示すが、これらは単なる例であって、本発明はこれ
らに限定されるものではない。Hereinafter, in order to explain the present invention in more detail, a method for producing a novel pharmaceutical according to the present invention and various physical properties of a product obtained thereby will be shown, but these are merely examples, and the present invention is not limited to these. isn't it.

艮−１し」１ 実施例　１ ヒドロフルメチアジドの調製 エタノール５０部中に、ヒドロフルメチアジド（ｈｙｄ
ｒｏｆｌｕｌｅｔｈｉａｚｌｄｅ）　１部及びポリビニ
ルピロリドン（ＰＶＰ）０．１部を溶解させる。この溶
液を次いで微粒子化（例えばＢＵＣＨｌ　　１９０装置
内）する。供給温度を１３２℃に調節し、出口温度を９
８℃とする。微粒子化流速は７５０１／時間である。Example 1 Preparation of hydroflumethiazide Hydroflumethiazide (hydroflumethiazide) was added to 50 parts of ethanol.
1 part of Polyvinylpyrrolidone (PVP) and 0.1 part of Polyvinylpyrrolidone (PVP). This solution is then micronized (eg in a BUCHL 190 apparatus). Adjust the feed temperature to 132°C and the outlet temperature to 9
The temperature shall be 8℃. The atomization flow rate is 7501/hour.

ｗｉ１図は、微粒子化していないヒドロフルメチアジド
（曲線ａ　）　、ＰＶＰの存在下に微粒子化されたヒド
ロフルメチアジド（曲線ｂ）、ヒドロフ−〇− ルメチアジドを微粒子化後、１０％ＰＶＰと混合したも
の〈曲線Ｃ）及び本発明実施例１に従い微粒子化された
ヒドロフルメチアジド（曲線ｄ）のそれぞれの溶解性を
示すグラフである。Figure wi1 shows hydroflumethiazide not micronized (curve a), hydroflumethiazide micronized in the presence of PVP (curve b), and hydroflumethiazide micronized and mixed with 10% PVP. It is a graph showing the respective solubility of <curve C) and hydroflumethiazide micronized according to Example 1 of the present invention (curve d).

該第１図より、本発明によれば、医薬の溶解性を顕著に
改善できるのに対し、ヒドロフルメチアジド＋ＰＶＰ混
含物では、その効果は非常に低いことが明らかである。From FIG. 1, it is clear that according to the present invention, the solubility of the drug can be significantly improved, whereas the effect of the hydroflumethiazide + PVP mixture is very low.

実施例１で得られた製品は、少くとも４ケ月間その構造
に実質的変化はなかった。これに対し、ＰＶＰの不存在
下に微粒子化したヒドロフルメチアジドは、１２日後に
は完全に結晶形態に変換された。The product obtained in Example 1 did not undergo any substantial change in its structure for at least 4 months. In contrast, hydroflumethiazide micronized in the absence of PVP was completely converted to crystalline form after 12 days.

実施例　２ ジピリダモルの調製 ジビリダモル（ｄｌｐｙｒｉｄａｉｏｌｅ）　！量の０
％、５％、１０％、２０％及び３５％のＰＶＰを含む溶
液を、実施例１と同様にして調製し、微粒子化する。Example 2 Preparation of Dipyridamole Dipyridamole (dlpyridaiole)! quantity 0
%, 5%, 10%, 20% and 35% of PVP are prepared and micronized as in Example 1.

第２図は、得られた各製品のＸ線回折図である。FIG. 2 is an X-ray diffraction pattern of each product obtained.

該図よりジビリダモル−ＰＶＰ　（３：　１　）混合物
（曲線Ｍ）は、明らかに曲線５とは異なる回折曲線を示
していることが判る。尚第２図において、曲線１　ハＰ
　Ｖ　Ｐ　０％を、曲線２　ハＰ　Ｖ　Ｐ　５％を、曲
線３ｉ、１ＰＶＰ１０％ｆ、曲［１４Ｇｅｔ　Ｐ　Ｖ　
Ｐ　２０％を及び曲線５はＰＶＰ３０％をそれぞれ示す
。It can be seen from the figure that the divyridamole-PVP (3:1) mixture (curve M) clearly shows a diffraction curve different from curve 5. In addition, in Figure 2, curve 1 HaP
V P 0%, Curve 2 HaP V P 5%, Curve 3i, 1PVP10%f, Song [14Get P V
Curve 5 shows P 20% and PVP 30% respectively.

曲線５により示される製品の溶解性は、混合物（曲線Ｍ
）の２倍以上である。The solubility of the product shown by curve 5 is similar to that of the mixture (curve M
) is more than twice as large.

実施例３〜２５ 以下の医薬を利用することにより、実施例１及び２と略
々同様の結果が得られる。Examples 3-25 Substantially the same results as in Examples 1 and 2 can be obtained by using the following drugs.

ヒト０りロロチアジド シクロチアジド シクロベンチアジト ポリチアジド メチルドパ スビロノラク］〜ン キニジン シアナドール メトロニダゾール イブプロフェン ナプロキセン ■リスロマイシン グラフエニン フロセミド サロクテイジル（５ｕｌｏｃｔｉｄｉｌ）ニトロフラン
トイン インドメタシン フラボキサート（ｆｌａｖｏｘａｔｅ　）フエノバルビ
タン シフランデレート ケトプロフェン ナフチドロフリル及び トリアムテレン 上記の通り本発明によれば、いかなる適用方法及び実施
態様を採用しようとも、従来公知のそれに比し、長期に
亙り安定で且つ完全な溶解性を有する優れた医薬が得ら
れる。Nitrofurantoin Indomethacin Flavoxate Phenobarbi Tansifuranderate Ketoprofen Naftidrofuryl and Triamterene As described above, the present invention provides superior long-term stability and complete solubility compared to conventionally known methods, regardless of the application method and embodiment adopted. You can obtain a medicine that

本発明は上記で詳述した適用形態、使用！ｇｌｌに限定
されず、本発明の範囲を逸脱しない限り当業９− 省が容易に想到し得るすべての変形をも当然に包含する
ものである。The present invention has been described in detail above in its application form and use! The present invention is not limited to the present invention, but naturally includes all modifications that can be easily conceived by those skilled in the art as long as they do not depart from the scope of the present invention.

【図面の簡単な説明】[Brief explanation of the drawing]

第１図は本発明医薬の溶解性を示づグラフ及び第２図は
本発明医薬のＸ線回折図をそれぞれしめす。 （以　上） １０−FIG. 1 is a graph showing the solubility of the medicament of the present invention, and FIG. 2 is an X-ray diffraction diagram of the medicament of the present invention. (and above) 10-

Claims (1)

【特許請求の範囲】 ■　安定剤及び結晶成長抑制剤の存在下での微粒子化に
より得られ、不定形形態を有することを特徴とする高度
溶解性医薬。 ■　安定剤及び結晶成長抑制剤が、ポリビニルピロリド
ンから構成される特許請求の範囲第１項に記載の医薬。 ■　安定剤及び結晶成長抑制剤が、ポリエチレングリコ
ールーボリビニルビロリドン混合物から構成される特許
請求の範囲第１項に記載の医薬。 ■　微粒子化時の安定剤及び結晶成長抑制剤濃度が、有
効成分重量の１〜５０！量％である特許請求の範囲第１
項乃至第３項のいずれかに記載の医薬。 ■　溶媒中に有効成分、安定剤及び結晶成長抑制剤を溶
解し、必要に応じ加熱後、入口温度１１０〜１５０℃及
び出口温度８０〜１２０°Ｃの条件下に微粒子化するこ
とを特徴とする高度溶解性医薬の製造法。 ■　有効成分、安定剤及び結晶成長抑制剤を溶解させる
ための溶媒が水及び（又は）低分子銀アルコール（Ｃ＋
〜Ｇｔ　）である特許請求の範囲第５項に記載の方法。[Claims] (1) A highly soluble drug obtained by micronization in the presence of a stabilizer and a crystal growth inhibitor and characterized by having an amorphous form. (2) The medicament according to claim 1, wherein the stabilizer and crystal growth inhibitor are composed of polyvinylpyrrolidone. (2) The medicament according to claim 1, wherein the stabilizer and crystal growth inhibitor are composed of a polyethylene glycol-borivinyl pyrrolidone mixture. ■ The concentration of stabilizer and crystal growth inhibitor during micronization is 1 to 50 of the weight of the active ingredient! Claim 1 which is amount %
The medicament according to any one of Items 3 to 3. ■ It is characterized by dissolving the active ingredient, stabilizer, and crystal growth inhibitor in a solvent, heating if necessary, and turning it into fine particles under conditions of an inlet temperature of 110 to 150°C and an outlet temperature of 80 to 120°C. Method for manufacturing highly soluble pharmaceuticals. ■ The solvent for dissolving the active ingredient, stabilizer and crystal growth inhibitor is water and/or low molecular weight silver alcohol (C+
~Gt).
JP57204422A 1982-04-19 1982-11-19 High dissolubility medicine and manufacture Granted JPS58183615A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR8206646 1982-04-19
FR8206646A FR2525108B1 (en) 1982-04-19 1982-04-19 HIGH-SOLUBILITY MEDICINES AND PROCESS FOR OBTAINING THEM

Publications (2)

Publication Number Publication Date
JPS58183615A true JPS58183615A (en) 1983-10-26
JPH0341444B2 JPH0341444B2 (en) 1991-06-24

Family

ID=9273120

Family Applications (1)

Application Number Title Priority Date Filing Date
JP57204422A Granted JPS58183615A (en) 1982-04-19 1982-11-19 High dissolubility medicine and manufacture

Country Status (18)

Country Link
US (2) US4610875A (en)
JP (1) JPS58183615A (en)
AR (1) AR230183A1 (en)
AT (1) AT389813B (en)
AU (1) AU555579B2 (en)
BE (1) BE894942A (en)
CA (1) CA1225029A (en)
CH (1) CH655003A5 (en)
DE (1) DE3241097A1 (en)
ES (1) ES8505249A1 (en)
FR (1) FR2525108B1 (en)
GB (1) GB2119784B (en)
IE (1) IE54084B1 (en)
IT (1) IT1153099B (en)
LU (1) LU84468A1 (en)
NL (1) NL8204461A (en)
PT (1) PT75867B (en)
SE (1) SE8206697L (en)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05501563A (en) * 1989-11-18 1993-03-25 シエーリング・アグロケミカルズ・リミテツド Production of propenoic acid derivatives
JPH0648937A (en) * 1992-04-07 1994-02-22 Seitai Kagaku Kenkyusho:Kk Medical agent suitable for oral administration and its production
WO1997034601A1 (en) * 1996-03-18 1997-09-25 Eisai Co., Ltd. Drug compositions improved in solubility
JP2002521315A (en) * 1998-07-20 2002-07-16 スミスクライン・ビーチャム・コーポレイション In vivo potentiated formulation of eprosartan in solid oral dosage form
JP2003513904A (en) * 1999-11-12 2003-04-15 アボット・ラボラトリーズ Crystallization inhibitors in solid dispersants
JP2004500358A (en) * 1999-12-08 2004-01-08 ファルマシア　コーポレイション Celecoxib in the solid state with increased bioavailability
US6743443B1 (en) 1998-10-05 2004-06-01 Eisai Co., Ltd. Tablets immediately disintegrating in the oral cavity
JP2005501820A (en) * 2001-06-22 2005-01-20 ファイザー・プロダクツ・インク Pharmaceutical composition of adsorbate of amorphous drug
JP2010526860A (en) * 2007-05-16 2010-08-05 ホビオネ インテル リミテッド Method for obtaining a steroid phosphate compound
JP2012507495A (en) * 2008-11-04 2012-03-29 シプラ・リミテッド Tiotropium bromide with low crystallinity
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GB2119784B (en) 1986-04-03
IT8224368A0 (en) 1982-11-23
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PT75867A (en) 1982-12-01
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US4769236A (en) 1988-09-06
ES517444A0 (en) 1985-05-16
BE894942A (en) 1983-05-09
IE54084B1 (en) 1989-06-07
AU9043182A (en) 1983-10-27
IT1153099B (en) 1987-01-14
AR230183A1 (en) 1984-03-01
CH655003A5 (en) 1986-03-27
FR2525108A1 (en) 1983-10-21
US4610875A (en) 1986-09-09
IE822610L (en) 1983-10-19
NL8204461A (en) 1983-11-16
ES8505249A1 (en) 1985-05-16
PT75867B (en) 1986-01-21
FR2525108B1 (en) 1989-05-12
DE3241097A1 (en) 1983-10-20
GB2119784A (en) 1983-11-23
LU84468A1 (en) 1983-06-13
CA1225029A (en) 1987-08-04
ATA427282A (en) 1989-07-15
JPH0341444B2 (en) 1991-06-24
AU555579B2 (en) 1986-10-02
IT8224368A1 (en) 1984-05-23
SE8206697D0 (en) 1982-11-24
DE3241097C2 (en) 1989-04-13

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